Quercetin and its Modified Form for Allergies and More

Flavonoids are a group of plant pigments largely responsible for the colors of many fruits and flowers. Flavonoids are also responsible for the medicinal actions of foods, juices, herbs and bee pollen and are now known to be directly related to their flavonoid content.

As a class of compounds, flavonoids have been referred to as “nature’s biologic response modifiers” because of their ability to modify the body’s reaction to other compounds, such as allergens, viruses, and carcinogens, as evidenced by their anti-inflammatory, antiallergic, antiviral, and anticancer properties. In addition, flavonoids act as powerful antioxidants, providing remarkable protection against oxidative and free radical damage.

This brief review will focus on the use of quercetin and its more bioavailable modified form—enzymatically modified isoquercitrin (EMIQ).

Quercetin

Quercetin serves as the backbone structure for many other flavonoids, including the citrus flavonoids rutin, quercitrin, and hesperidin. These derivatives differ from quercetin in that they have sugar molecules attached to the quercetin backbone. Quercetin is consistently the most active of the flavonoids in experimental studies, and many medicinal plants owe much of their activity to their high quercetin content.

In preclinical studies, quercetin has demonstrated significant anti-inflammatory and antiallergic activity. It directly inhibits several of the initial steps of inflammation and allergy. For example, it inhibits both the manufacture and release of histamine and other allergic/inflammatory mediators. In addition it exerts potent antioxidant activity. Based on these test tube studies, quercetin is often recommended for use in virtually all sorts of inflammatory and allergic conditions, however there is a lack of clinical studies in these applications with regular quercetin. In a study using EMIQ, very good results were achieved in hay fever (discussed below).

Before discussing the clinical results with quercetin, it is important to address its absorption and metabolism. In human absorption studies, quercetin has been shown to be poorly absorbed with a high degree of variability from one person to the next. Results appear most likely to occur at relatively high dosage levels (e.g., 1,000 mg per day) or by using EMIQ to overcome these shortcomings.

One of the first clinical studies with quercetin was a double-blind study in nonbacterial chronic prostatitis (inflammation of the prostate gland). This condition is characterized by chronic pelvic pain that is worse upon urination. In patients taking quercetin (500 mg twice daily), more than 67 percent had an improvement of symptoms of at least 25 percent. Combining quercetin with bromelain (discussed under in Available Forms) produced even better results (82 percent had at least a 25 percent improvement in symptom score).

By far the most popular application for quercetin is in beverages designed for athletic performance. The commercial success of this application led to significant scientific investigation of quercetin’s ability to improve physical performance. In a number of clinical trials, quercetin was shown to improve mental/physical performance and reduce infection risk.

In one study, of 40 trained male cyclists who received quercetin or placebo before, during, and for two weeks, after a three-day period in which subjects cycled for three hours/day at approximately 57 percent maximal workload, only one of 20 developed upper respiratory infection symptoms in the quercetin group compared with nine of 20 in the placebo group. In another study, reduction in upper respiratory tract infection total sick days and severity was noted in middle aged and older subjects ingesting 1000 mg/day quercetin for 12 weeks who rated themselves as physically fit.

EMIQ

EMIQ is manufactured through a natural enzymatic modification that attaches glucose chains (glycosides) to the quercetin molecule. The result of this modification greatly enhances quercetin bioavailability. In the digestive process the glycoside portion is cleaved liberating the quercetin and as a result EMIQ greatly increases quercetin levels in the blood compared to the ingestion of quercetin or its related compound rutin. Blood levels of quercetin are more than 40 times greater with EMIQ compared to an equal amount of quercetin. Hence, 50 mg of EMIQ would be equal to approximately 1,000 mg of quercetin. Most clinical studies have used a dosage of 200 mg daily of EMIQ. That level would be equal to a whopping 8,000 mg of quercetin.

In Japan, research has shown EMIQ is useful in helping reduce the major symptoms of hay fever. In these double- blind, placebo-controlled studies, subjects suffering from allergy to Japanese cedar pollen, took two capsules daily of 100 mg EMIQ or a placebo for eight weeks during the pollen season. Throughout the course of the study, EMIQ group experienced significantly less red, itchy eyes.

EMIQ also exerts significant effects in reducing body fat accumulation including abdominal (visceral or “belly fat”). The mechanism of action is the promotion of enzymes that promote the breakdown of fat within fat cells. In the first human double blind study, 200 overweight and obese subjects (102 men and 98 women) were randomly divided into two groups and ingested a beverage containing 0 mg or 275 mg of EMIQ for 12 weeks. Abdominal total fat area, visceral fat area, subcutaneous fat area and waist circumference reduced significantly in test group compared to placebo group. The overall reduction in body fat was over 20 percent. A second study by the same research group showed that a dosage of 110 mg per day produced similar benefits.

Available Forms

Quercetin is available alone in powder, tablet, and capsule form as well as in beverages. However, if quercetin is being used for its anti-inflammatory properties, products that combine with an equal amount of the pineapple enzyme bromelain may provide additional benefit. Bromelain exerts anti-allergy and anti-inflammatory activity on its own and may also enhance the absorption of quercetin. Combination preparations of proteindigesting enzymes, like bromelain, and flavonoids have been shown to potentiate each other’s anti-inflammatory activity.

EMIQ is also available in beverages as well as in capsules or tablets. It is absorbed very well on its own, so it is not necessary to combine it with bromelain.

Safety and Drug Interactions

Both quercetin and EMIQ are well tolerated in humans with no side effects noted in the clinical studies. Animal studies have also showed that quercetin and EMIQ have no apparent side effects, even when consumed in large quantities for long periods of time (up to two years). EMIQ has generally recognized as safe (GRAS) status in the United States.

Quercetin and EMIQ may enhance the uptake from the intestine of certain drugs, including vinblastine, cyclosporine, digoxin, fexofenadine, losartan, nifedipine, felodipine, verapamil, and terfenadine. Lower dosage of these drugs may be required to avoid toxicity.

Dr. Michael Murray
7/15/2016

Welcome

On the Dr Oz show

On the show I discussed the failure of conventional medicine to address the underlying issues in many health conditions offering little more than drugs as biochemical “band aids.”

December is Seasonal Affective Disorder Awareness Month

In seasonal affective disorder (SAD) is associated with winter depression Typically, these individuals not only feel depressed they also feel tried, slow down, and generally oversleep, overeat, and crave carbohydrates in the winter. In the summer, these same patients feel very good and maybe even are elated, active, and energetic.

Although many variables may be responsible for SAD, insufficient light exposure is the most logical explanation. Many mammals exhibit seasonal variations in activity level, sleep patterns, and appetite and are extremely sensitive to changes in day length. The antidepressant effects of full-spectrum light therapy have been demonstrated in well-monitored, controlled studies in SAD. The antidepressant effect of light therapy is probably due to the restoration of proper melatonin synthesis and secretion by the pineal gland, leading to reestablishment of the proper circadian rhythm. Full-spectrum white light (10,000 lux) is prescribed for at least 30 minutes every day in the morning. Or, better yet, use full-spectrum lighting throughout the indoor environment.

The key hormonal change caused by exposure to full spectrum lighting may be a reduced secretion of melatonin from the pineal gland and an increased secretion of cortisol by the adrenal glands. Melatonin supplementation is thought to improve SAD because it increases brain melatonin levels, but it may also suppress cortisol secretion.Take 3-5 mg 45 minutes before retiring.

Vitamin D is also an important consideration. Many experts recommend a dosage of 2,000 to 5,000 IU of vitamin D3 daily, especially during the winter months.

Mind Your Ps and Qs

PQQ may be the perfect answer to preventing or reversing age-related mental decline.

kiwiPQQ (short for pyrroloquinoline quinone) is a vitamin-like compound found in plant foods that shows a wide range of benefits for brain function and energy production. Learn more about PQQ with the following Q&A.
What Exactly Does PQQ Do?

PQQ is an extremely potent antioxidant that is able to carry out the role of an antioxidant in the body more than 20,000 times—which is a rare thing. For example, other antioxidants, such as vitamin C, are only able to accomplish this “cycling” process about four times.
Are There Any Food Sources of PQQ?

PQQ has been found in all plant foods analyzed to date. Particularly PPQ-rich foods include parsley, green peppers, kiwi, papaya, and tofu. These foods contain 2–3 mcg of PQQ per 100 grams. Green tea provides about the same amount per 4-oz. serving. While these amounts appear to be sufficient in helping our cells carry out their basic functions, research indicates that boosting PQQ through supplementation can produce some amazing effects.